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Literature summary for 2.5.1.10 extracted from

  • Gisselberg, J.E.; Herrera, Z.; Orchard, L.M.; Llinas, M.; Yeh, E.
    Specific inhibition of the bifunctional farnesyl/geranylgeranyl diphosphate synthase in Malaria parasites via a new small-molecule binding site (2018), Cell Chem. Biol., 25, 185-193 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.5.1.10

Protein Variants

Protein Variants Comment Organism
s228T inhibition of the bifunctional farnesyl/geranylgeranyl diphosphate synthase by MMV019313, but not bisphosphonates, is disrupted in an S228T variant Plasmodium falciparum

Inhibitors

Inhibitors Comment Organism Structure
MMV019313 the inhibitor is highly selective for Plasmodium falciparum FPPS/GGPPS and shows no activity against human farnesyl diphosphate synthase or geranylgeranyl diphosphate synthase. Inhibition of the bifunctional farnesyl/geranylgeranyl diphosphate synthase by MMV019313, but not bisphosphonates, is disrupted in an S228T variant, demonstrating that MMV019313 and bisphosphonates have distinct modes-of-inhibition. Inhibition occurs via a new small molecule binding site Plasmodium falciparum

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate Plasmodium falciparum reaction of EC 2.5.1.29, bifunctional farnesyl/geranylgeranyl diphosphate synthase diphosphate + geranylgeranyl diphosphate
-
 ?
geranyl diphosphate + isopentenyl diphosphate Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8II79
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(2E,6E)-farnesyl diphosphate + isopentenyl diphosphate reaction of EC 2.5.1.29, bifunctional farnesyl/geranylgeranyl diphosphate synthase Plasmodium falciparum diphosphate + geranylgeranyl diphosphate
-
 ?
geranyl diphosphate + isopentenyl diphosphate bifunctional farnesyl/geranylgeranyl diphosphate synthase Plasmodium falciparum diphosphate + (2E,6E)-farnesyl diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
bifunctional farnesyl/geranylgeranyl diphosphate synthase
-
 Plasmodium falciparum
FPPS/GGPPS
-
 Plasmodium falciparum

General Information

General Information Comment Organism
drug target antimalarial drug target Plasmodium falciparum
metabolism the bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) is a key branchpoint enzyme in isoprenoid biosynthesis in Plasmodium falciparum (malaria) parasites Plasmodium falciparum